CA2795157C - Raltegravir salts and crystalline forms thereof - Google Patents

Raltegravir salts and crystalline forms thereof Download PDF

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Publication number
CA2795157C
CA2795157C CA2795157A CA2795157A CA2795157C CA 2795157 C CA2795157 C CA 2795157C CA 2795157 A CA2795157 A CA 2795157A CA 2795157 A CA2795157 A CA 2795157A CA 2795157 C CA2795157 C CA 2795157C
Authority
CA
Canada
Prior art keywords
raltegravir
theta
degrees
ray powder
potassium
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
CA2795157A
Other languages
English (en)
French (fr)
Other versions
CA2795157A1 (en
Inventor
Ana Kwokal
Lilach Hedvati
Revital Burstein
Adi Yeori
Rinat Moshkovits-Kaptsan
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Teva Pharmaceutical Industries Ltd
Original Assignee
Teva Pharmaceutical Industries Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Teva Pharmaceutical Industries Ltd filed Critical Teva Pharmaceutical Industries Ltd
Publication of CA2795157A1 publication Critical patent/CA2795157A1/en
Application granted granted Critical
Publication of CA2795157C publication Critical patent/CA2795157C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Communicable Diseases (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Crystals, And After-Treatments Of Crystals (AREA)
  • Developing Agents For Electrophotography (AREA)
CA2795157A 2010-04-01 2011-04-01 Raltegravir salts and crystalline forms thereof Active CA2795157C (en)

Applications Claiming Priority (15)

Application Number Priority Date Filing Date Title
US32006210P 2010-04-01 2010-04-01
US61/320,062 2010-04-01
US32692210P 2010-04-22 2010-04-22
US61/326,922 2010-04-22
US32928410P 2010-04-29 2010-04-29
US61/329,284 2010-04-29
US35339810P 2010-06-10 2010-06-10
US61/353,398 2010-06-10
US39275910P 2010-10-13 2010-10-13
US39277010P 2010-10-13 2010-10-13
US61/392,770 2010-10-13
US61/392,759 2010-10-13
US41763210P 2010-11-29 2010-11-29
US61/417,632 2010-11-29
PCT/US2011/030892 WO2011123754A1 (en) 2010-04-01 2011-04-01 Raltegravir salts and crystalline forms thereof

Publications (2)

Publication Number Publication Date
CA2795157A1 CA2795157A1 (en) 2011-10-06
CA2795157C true CA2795157C (en) 2015-11-24

Family

ID=44041698

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2795157A Active CA2795157C (en) 2010-04-01 2011-04-01 Raltegravir salts and crystalline forms thereof

Country Status (10)

Country Link
US (3) US20130079360A1 (de)
EP (2) EP2796458B1 (de)
JP (1) JP5889275B2 (de)
KR (1) KR101471735B1 (de)
CA (1) CA2795157C (de)
ES (2) ES2659549T3 (de)
PT (1) PT2545048E (de)
RU (1) RU2012146517A (de)
SI (2) SI2796458T1 (de)
WO (1) WO2011123754A1 (de)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012103105A1 (en) 2011-01-24 2012-08-02 Assia Chemical Industries Ltd. Processes for preparing raltegravir and intermediates in the processes
WO2012137142A1 (en) * 2011-04-06 2012-10-11 Lupin Limited Novel salts of raltegravir
EP2522665A1 (de) * 2011-05-03 2012-11-14 Sandoz Ag Kristallinnatriumsalz eines HIV-Integrasehemmers
EP2529741B1 (de) * 2011-06-01 2014-02-12 Ratiopharm GmbH Zusammensetzung und Tablette beinhaltend Raltegravir
WO2013037731A1 (de) * 2011-09-16 2013-03-21 Hexal Ag Neue polymorphe form von raltegravir-kalium
KR20140114406A (ko) * 2012-01-25 2014-09-26 루핀 리미티드 안정한 비정질 랄테그라빌 포타슘 프리믹스 및 이의 제조 방법
EP2875024A4 (de) * 2012-07-20 2015-12-23 Merck Sharp & Dohme Hiv-behandlung mit amidosubstituierten pyrimidinonderivaten
EP2818470A1 (de) * 2013-06-27 2014-12-31 Basf Se Kokristalle von Raltegravir-Kalium
WO2015140765A1 (en) 2014-03-21 2015-09-24 Mylan Laboratories Ltd. A premix of crystalline raltegravir potassium salt and a process for the preparation thereof
WO2017001996A1 (en) * 2015-06-29 2017-01-05 Laurus Labs Private Limited A process for preparing raltegravir potassium form 3
CN108292605B (zh) * 2016-06-24 2021-08-27 富士电机株式会社 半导体装置的制造方法和半导体装置
US10752618B2 (en) * 2016-09-15 2020-08-25 Lupin Limited Process for the preparation of pure and stable crystalline Raltegravir potassium form 3

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL212914B1 (pl) 2001-10-26 2012-12-31 Angeletti P Ist Richerche Bio N-podstawione hydroksypirymidynonokarboksyamidy jako inhibitory integrazy HIV
UA87884C2 (uk) * 2004-12-03 2009-08-25 Мерк Энд Ко., Инк. Безводна кристалічна калієва сіль інгібітора віл-інтегрази
WO2006060681A2 (en) * 2004-12-03 2006-06-08 Merck & Co., Inc. Pharmaceutical composition containing an anti-nucleating agent
WO2010140156A2 (en) 2009-06-02 2010-12-09 Hetero Research Foundation Novel polymorphs of raltegravir potassium
WO2011024192A2 (en) 2009-07-27 2011-03-03 Matrix Laboratories Ltd Novel polymorphs of raltegravir
US8962833B2 (en) * 2010-05-25 2015-02-24 Hetero Research Foundation Salts of raltegravir

Also Published As

Publication number Publication date
EP2796458B1 (de) 2018-01-10
CA2795157A1 (en) 2011-10-06
ES2524380T3 (es) 2014-12-05
SI2545048T1 (sl) 2014-12-31
KR101471735B1 (ko) 2014-12-10
WO2011123754A1 (en) 2011-10-06
KR20120139763A (ko) 2012-12-27
EP2796458A1 (de) 2014-10-29
US20130079360A1 (en) 2013-03-28
US20130096147A1 (en) 2013-04-18
ES2659549T3 (es) 2018-03-16
PT2545048E (pt) 2014-11-28
SI2796458T1 (en) 2018-04-30
EP2545048B1 (de) 2014-10-08
EP2545048A1 (de) 2013-01-16
JP2013523771A (ja) 2013-06-17
US20140256755A1 (en) 2014-09-11
RU2012146517A (ru) 2014-05-10
US8722722B2 (en) 2014-05-13
JP5889275B2 (ja) 2016-03-22

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